Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors

被引:24
作者
Sakamuri, S
Enyedy, IJ
Kozikowski, AP
Zaman, WA
Johnson, KM
Wang, SM
机构
[1] Georgetown Univ, Med Ctr, Drug Discovery Program, Washington, DC 20007 USA
[2] Georgetown Univ, Med Ctr, Dept Neurol, Washington, DC 20007 USA
[3] Georgetown Univ, Med Ctr, Dept Oncol, Washington, DC 20007 USA
[4] Georgetown Univ, Med Ctr, Dept Neurosci, Washington, DC 20007 USA
[5] Univ Texas, Med Branch, Dept Pharmacol & Toxicol, Galveston, TX 77555 USA
关键词
D O I
10.1016/S0960-894X(00)00703-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:495 / 500
页数:6
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